Title (en)

THROMBIN RECEPTOR ANTAGONISTS

Title (de)

ANTAGONISTEN GEGEN DEN THROMBINREZEPTOR

Title (fr)

ANTAGONISTES DE RECEPTEURS DE LA THROMBINE

Publication

EP 0656008 B1 20000315 (EN)

Application

EP 93917028 A 19930708

Priority

• US 9306428 W 19930708
• US 92234092 A 19920730
• US 8078893 A 19930628

Abstract (en)

[origin: US5866681A] Peptide derivatives serving as thrombin receptor antagonists are disclosed, which bear specificity for the cellular thrombin receptor without interfering with the catalytic activities of thrombin. The derivatives generally have the formula <IMAGE>kylamide linkages, or isosteric replacements of such linkages; R2 is either a neutral amino acid side chain or a hydrophobic radical; R4 is hydrophobic radical; R5 is CO, CH2 or SO; X is either of the formula: <IMAGE> in which R6 and R7 are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R8 is a hydrophobic radical, or a hydrophobic residue; Y is alkoxy, hydroxy, amino, alkylamino, dialkylamino, in which any of the alkyl groups may be substituted with a basic moiety; Z is an amino acid or peptide residue; and m is zero or one.

IPC 1-7

C07K 5/06; C07K 5/10; C07K 7/06

IPC 8 full level

A61K 38/00 (2006.01); A61P 7/02 (2006.01); A61P 9/08 (2006.01); A61P 9/10 (2006.01); A61P 29/00 (2006.01); C07K 5/062 (2006.01); C07K 5/065 (2006.01); C07K 5/083 (2006.01); C07K 5/087 (2006.01); C07K 5/103 (2006.01); C07K 5/107 (2006.01); C07K 7/02 (2006.01); C07K 7/06 (2006.01); C07K 7/08 (2006.01)

CPC (source: EP US)

A61P 7/02 (2018.01 - EP); A61P 9/08 (2018.01 - EP); A61P 9/10 (2018.01 - EP); A61P 29/00 (2018.01 - EP); C07K 5/06078 (2013.01 - EP US); C07K 5/1016 (2013.01 - EP US); C07K 7/02 (2013.01 - EP US); C07K 7/06 (2013.01 - EP US); A61K 38/00 (2013.01 - EP US)

Designated contracting state (EPC)

AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL PT SE

DOCDB simple family (publication)

US 5866681 A 19990202; AT E190625 T1 20000415; AU 4668593 A 19940303; AU 669922 B2 19960627; CA 2140543 A1 19940217; CA 2140543 C 20010410; DE 69328104 D1 20000420; DE 69328104 T2 20001221; EP 0656008 A1 19950607; EP 0656008 B1 20000315; IL 106197 A0 19940530; IL 106197 A 19991130; JP 2675438 B2 19971112; JP H07506115 A 19950706; SG 49772 A1 19980615; WO 9403479 A1 19940217

DOCDB simple family (application)

US 40746895 A 19950320; AT 93917028 T 19930708; AU 4668593 A 19930708; CA 2140543 A 19930708; DE 69328104 T 19930708; EP 93917028 A 19930708; IL 10619793 A 19930630; JP 50531094 A 19930708; SG 1996005407 A 19930708; US 9306428 W 19930708